TAK-960 monohydrochloride is an orally available compound that selectively inhibits polo-like kinase 1 (PLK1) with an IC 50 of 0.8 nM. It also demonstrates inhibitory activity against PLK2 (IC 50 of 16.9 nM) and PLK3 (IC 50 of 50.2 nM). Moreover, TAK-960 monohydrochloride effectively suppresses the proliferation of various cancer cell lines and exhibits significant efficacy against multiple tumor xenografts.